Synthesis, Preliminary Bioevaluation and Computational Analysis of Caffeic Acid Analogues

被引：7

作者：

Liu, Zhiqian ^{[1
]}

Fu, Jianjun ^{[2
]}

Shan, Lei ^{[1
]}

Sun, Qingyan ^{[1
]}

Zhang, Weidong ^{[1
]}

机构：

[1] Second Mil Med Univ, Dept Phytochem, Sch Pharm, Shanghai 200433, Peoples R China

[2] E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2014年 / 15卷 / 05期

基金：

中国国家自然科学基金;

关键词：

anti-inflammatory; caffeic acid amides; synthesis; pharmacophore; target predication; NITRIC-OXIDE PRODUCTION; INFLAMMATION; INHIBITORS;

D O I：

10.3390/ijms15058808

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of caffeic acid amides were designed, synthesized and evaluated for anti-inflammatory activity. Most of them exhibited promising anti-inflammatory activity against nitric oxide (NO) generation in murine macrophage RAW264.7 cells. A 3D pharmacophore model was created based on the biological results for further structural optimization. Moreover, predication of the potential targets was also carried out by the PharmMapper server. These amide analogues represent a promising class of anti-inflammatory scaffold for further exploration and target identification.

引用

页码：8808 / 8820

页数：13

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